Trimethoprim lactate

SKU: orb1691000

Description

Trimethoprim lactate is a dihydrofolate reductase (DHFR) inhibitor antibiotic effective against Gram-negative bacteria. It is utilized in research for studying bacterial infections and antimicrobial mechanisms, both in vitro and in vivo, particularly for ocular, pulmonary, and gastrointestinal tract models.

Research Area

Cell Biology, Infectious Disease & Virology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 23256-42-0
• MW: 380.4
• Purity: 99.90% (May vary between batches)
• Formula: C₁₇H₂₄N₄O₆
• SMILES: O=C(O)C(O)C.N=1C=C(C(=NC1N)N)CC2=CC(OC)=C(OC)C(OC)=C2
• Target: Antibiotic,Antibacterial,Antifolate
• Solubility: DMSO:200 mg/mL (525.76 mM);H2O:10 mg/mL (26.29 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (13.14 mM)

Bioactivity

• In Vivo:
  In an intraperitoneal infection assay in mice, the CD50 values of Trimethoprim lactate against Haemophilus influenzae, Streptococcus pneumoniae, Escherichia coli, and Neisseria meningitidis were 150 mg/kg, 335 mg/kg, 27.5 mg/kg, and 8.4 mg/kg, respectively. When conjugated with thiomaltose (TM-TMP), Trimethoprim lactate maintains stability in complete serum, with a half-life of approximately one hour, and shows an MIC of about 1 μM against E. coli .
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• In Vitro:
  Trimethoprim lactate interferes with folate metabolism by inhibiting dihydrofolate reductase (DHFR) activity, thereby preventing the reduction of dihydrofolate to tetrahydrofolate (THF). In E. coli cells, Trimethoprim lactate causes protein aggregation and induces major heat shock proteins (Hsps), suggesting that its presence leads to protein misfolding.Trimethoprim lactate induces the expression of the heat shock proteins DnaK, DnaJ, GroEL, ClpB, and IbpA/B, of which IbpA/B was most significantly induced and co-aggregated with insoluble proteins.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Primsol lactate, NIH204 lactate, NIH 204 lactate, NSC-106568 lactate, Bacterial, BW56-72 lactate, BW 56-72 lactate, Antibiotic, Antifolate

Compound Identifiers

PubChem CID

3084396